AR019167A1 - HETEROAROMATIC DERIVATIVES OF PIPERAZINAS DI-N-SUBSTITUTED AND PIPERIDINES 1,4-DISUSTITUTED, PHARMACEUTICAL COMPOSITIONS AND THE USE OF THE SAME FOR THE PREPARATION OF MEDICINES - Google Patents

HETEROAROMATIC DERIVATIVES OF PIPERAZINAS DI-N-SUBSTITUTED AND PIPERIDINES 1,4-DISUSTITUTED, PHARMACEUTICAL COMPOSITIONS AND THE USE OF THE SAME FOR THE PREPARATION OF MEDICINES

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Publication number
AR019167A1
AR019167A1 ARP990103104A ARP990103104A AR019167A1 AR 019167 A1 AR019167 A1 AR 019167A1 AR P990103104 A ARP990103104 A AR P990103104A AR P990103104 A ARP990103104 A AR P990103104A AR 019167 A1 AR019167 A1 AR 019167A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
substituted
preparation
pharmaceutical compositions
Prior art date
Application number
ARP990103104A
Other languages
Spanish (es)
Original Assignee
Schering Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Publication of AR019167A1 publication Critical patent/AR019167A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los derivados heterocíclicos de los compuestos de piperazina di-N-sustituida o piperidina, 1,4 di-sustituida de acuerdo con la formula I(incluyendo a todoslos isomeros, sales y solvatos) donde uno de Y y Z es -N- y el otro es -N- o -CH-; X es -O-,-S -, -SO-, -SO2 -o -CH2, Q es formula II, R es alquilo (C1-20),cicloalquilo (C3-12) arilo, R8-arilo o heteroarilo; R1, R2 y R3 se seleccionan independientemente del grupo formado por H y alquilo (C1-20); R4 es alquilo (C1-20), cicloalquilo (C3-C12)o f ormula III, R5 es H, alquilo (C1-20), -C(O)alquilo (C1-20), R9-arilcarbonilo, -SO2-alquilo(C1-29), R9-arilsulfonilo-C(O)Oalquilo(C1-20), R9-ariloxi-carbonilo, -C(O)NH-alquilo(C1-20) o R9-arilaminocarbonilo; R6 es H, o alquilo (C1-20); R7 es H,alquil o(C1-20), hidroxialquilo (C1-20) o alcoxi(C1-20)-alquilo(C1-20); R8 es 1-3 sustituyentes seleccionados independientemente del grupo formado por H, alquilo (C1-10),halogeno,hidroxi, alcoxi (C1-20) ohidroxi(C1-20)alquilo, o dos grupos R8adyacentes pue den unirse para formar un grupo alquilendioxi (C1-2); y R9 es 1-3 sustituyentes independientementeseleccionados del grupo formado por H, alquilo (C1-20), halogeno, amino o alquilamino (C1-20). Son antagonistas muscarínicos utiles paratratar los tras tornoscognoscitivos como por ejemplo la enfermedad de Alzheimer. También se describen las composiciones farmacéuticas y el uso de dichos derivados para lapreparacion de un medicamento.The heterocyclic derivatives of the di-N-substituted piperazine or piperidine, 1,4-di-substituted compounds according to formula I (including all isomers, salts and solvates) where one of Y and Z is -N- and the another is -N- or -CH-; X is -O -, - S -, -SO-, -SO2 -or -CH2, Q is formula II, R is (C1-20) alkyl, (C3-12) cycloalkyl, aryl, R8-aryl or heteroaryl; R1, R2 and R3 are independently selected from the group consisting of H and (C1-20) alkyl; R4 is (C1-20) alkyl, (C3-C12) cycloalkyl of formula III, R5 is H, (C1-20) alkyl, -C (O) (C1-20) alkyl, R9-arylcarbonyl, -SO2-alkyl (C1-29), R9-arylsulfonyl-C (O) Oalkyl (C1-20), R9-aryloxycarbonyl, -C (O) NH-alkyl (C1-20) or R9-arylaminocarbonyl; R6 is H, or (C1-20) alkyl; R7 is H, alkyl or (C1-20), hydroxyalkyl (C1-20) or (C1-20) alkoxy-(C1-20) alkyl; R8 is 1-3 substituents independently selected from the group consisting of H, (C1-10) alkyl, halogen, hydroxy, (C1-20) alkoxy or (C1-20) alkyl, or two adjacent R8 groups can be joined to form a group (C1-2) alkylenedioxy; and R9 is 1-3 substituents independently selected from the group consisting of H, (C1-20) alkyl, halogen, amino or (C1-20) alkylamino. They are useful muscarinic antagonists to treat the after-stenosis, such as Alzheimer's disease. Pharmaceutical compositions and the use of such derivatives for the preparation of a medicament are also described.

ARP990103104A 1998-06-30 1999-06-28 HETEROAROMATIC DERIVATIVES OF PIPERAZINAS DI-N-SUBSTITUTED AND PIPERIDINES 1,4-DISUSTITUTED, PHARMACEUTICAL COMPOSITIONS AND THE USE OF THE SAME FOR THE PREPARATION OF MEDICINES AR019167A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10798398A 1998-06-30 1998-06-30

Publications (1)

Publication Number Publication Date
AR019167A1 true AR019167A1 (en) 2001-12-26

Family

ID=22319562

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990103104A AR019167A1 (en) 1998-06-30 1999-06-28 HETEROAROMATIC DERIVATIVES OF PIPERAZINAS DI-N-SUBSTITUTED AND PIPERIDINES 1,4-DISUSTITUTED, PHARMACEUTICAL COMPOSITIONS AND THE USE OF THE SAME FOR THE PREPARATION OF MEDICINES

Country Status (17)

Country Link
EP (1) EP1091956B1 (en)
JP (1) JP3344997B2 (en)
KR (1) KR20010053254A (en)
CN (1) CN1146559C (en)
AR (1) AR019167A1 (en)
AT (1) ATE272632T1 (en)
AU (1) AU756484B2 (en)
CA (1) CA2336000C (en)
DE (1) DE69919171T2 (en)
ES (1) ES2221399T3 (en)
HU (1) HUP0104058A2 (en)
IL (1) IL140249A0 (en)
MY (1) MY133108A (en)
NZ (1) NZ508910A (en)
TW (1) TW474933B (en)
WO (1) WO2000000488A1 (en)
ZA (1) ZA200007555B (en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6391865B1 (en) 1999-05-04 2002-05-21 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
US6689765B2 (en) 1999-05-04 2004-02-10 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
US6635646B1 (en) 1999-05-04 2003-10-21 Schering Corporation Pegylated interferon alfa-CCR5 antagonist combination HIV therapy
SK286641B6 (en) * 1999-05-04 2009-03-05 Schering Corporation Piperazine derivatives useful as CCR5 antagonists, pharmaceutical compositions comprising them and their use
ATE264301T1 (en) * 1999-09-22 2004-04-15 Schering Corp MUSCARINE ANTAGONISTS
US6294554B1 (en) 1999-09-22 2001-09-25 Schering Corporation Muscarinic antagonists
AR033517A1 (en) 2000-04-08 2003-12-26 Astrazeneca Ab PIPERIDINE DERIVATIVES, PROCESS FOR THE PREPARATION AND USE OF THESE DERIVATIVES IN THE MANUFACTURE OF MEDICINES
US6849621B2 (en) 2001-03-13 2005-02-01 Schering Corporation Piperidine compounds
BR0210733A (en) 2001-07-02 2004-07-20 Astrazeneca Ab Useful piperidine derivatives useful as modulators of chemokine receptor activity
GB0120461D0 (en) 2001-08-22 2001-10-17 Astrazeneca Ab Novel compounds
GB0122503D0 (en) 2001-09-18 2001-11-07 Astrazeneca Ab Chemical compounds
SE0200844D0 (en) 2002-03-19 2002-03-19 Astrazeneca Ab Chemical compounds
SE0200843D0 (en) 2002-03-19 2002-03-19 Astrazeneca Ab Chemical compounds
SE0202838D0 (en) * 2002-09-24 2002-09-24 Astrazeneca Ab Chemical compounds
SE0300957D0 (en) 2003-04-01 2003-04-01 Astrazeneca Ab Chemical compounds
US20080200505A1 (en) * 2005-05-27 2008-08-21 Astrazeneca Ab Piperidines for the Treatment of Chemokine Mediated Diseases
TW200722419A (en) * 2005-05-27 2007-06-16 Astrazeneca Ab Chemical compounds
CA2615650A1 (en) 2005-07-21 2007-01-25 Astrazeneca Ab Novel piperidine derivatives
US8536168B2 (en) 2007-03-15 2013-09-17 Novartis Ag Benzyl and pyridinyl derivatives as modulators of the hedgehog signaling pathway
US20100041663A1 (en) 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
CN104356056B (en) * 2014-11-19 2017-04-05 南京华威医药科技开发有限公司 The preparation method of pyrrole Lun Panai intermediate

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL117149A0 (en) * 1995-02-23 1996-06-18 Schering Corp Muscarinic antagonists

Also Published As

Publication number Publication date
KR20010053254A (en) 2001-06-25
EP1091956B1 (en) 2004-08-04
ZA200007555B (en) 2002-03-15
JP2002519349A (en) 2002-07-02
JP3344997B2 (en) 2002-11-18
ES2221399T3 (en) 2004-12-16
NZ508910A (en) 2003-01-31
CA2336000A1 (en) 2000-01-06
WO2000000488A1 (en) 2000-01-06
ATE272632T1 (en) 2004-08-15
HUP0104058A2 (en) 2002-03-28
EP1091956A1 (en) 2001-04-18
AU4820199A (en) 2000-01-17
MY133108A (en) 2007-10-31
DE69919171D1 (en) 2004-09-09
CA2336000C (en) 2006-10-10
AU756484B2 (en) 2003-01-16
DE69919171T2 (en) 2005-08-04
CN1146559C (en) 2004-04-21
TW474933B (en) 2002-02-01
CN1314905A (en) 2001-09-26
IL140249A0 (en) 2002-02-10

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